Table 3

Steady-state galunisertib pharmacokinetic parameters following multiple doses

Galunisertib 50 mg one time per day+durvalumab 1500 mg Q4WGalunisertib 50 mg two times per day+durvalumab 1500 mg Q4WGalunisertib 80 mg two times per day+durvalumab 1500 mg Q4WGalunisertib 150 mg two times per day+durvalumab 1500 mg Q4W
Patients per cohort34332
PK-evaluable patients*32325
PK profiles63638
Cycle 1 profiles32324
Cycle 2 profiles31314
tmax, hours, median (range)0.6 (0.5–3.9)0.5 (0.5–0.9)3.8 (0.5–4.0)2.7 (0.5–4.0)
Cmax, µmol/L424 (70)260† (71)612 (39)1070 (83)
AUC(0-tau), µg·h/L1630 (32)
(tau=24 hours)
813 (68)
(tau=12 hours)
3150 (63)
(tau=12 hours)
6120 (58)
(tau=12 hours)
  • All PK parameters at steady state are geometric mean (CV %) unless stated otherwise.

  • *Patients with ≥1 profile of day 14 pre-dose sample, two post-dose samples, and 1 day 15 pre-dose (24-hour) sample.

  • †Should be interpreted with caution due to limited data (n=3). There is overlap between the observed Cmax ranges following galunisertib 50 mg one time per day and 50 mg two times per day administration (see online supplemental figure S2).

  • AUC(0-tau), area under the concentration versus time curve for the dosing interval; Cmax, maximum observed concentration; CV, coefficient of variation; PK, pharmacokinetics; Q4W, every 4 weeks; tmax, time of maximum observed concentration.